Sunitinib

For research use only. Not for use in humans.

製品コードS7781 別名:SU11248

Sunitinib化学構造

CAS No. 557795-19-4

Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.

サイズ 価格(税別)  
JPY 18100
JPY 34700
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バルク問合せ

文献中Selleckの製品使用例(156)

製品安全説明書

PDGFR阻害剤の選択性比較

生物活性

製品説明 Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
ターゲット
FLT3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
体外試験

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC cell NHHrOHZHfW6ldHnvckBie3OjeR?= NGj4boszPCCq M4i0OGlvcGmkaYTpc44hd2ZiVlXHSk1CKGmwZIXj[YQhUFWYRVOgZ4VtdCC|cILveZRqdmdiYX\0[ZIhOjRiaILzJIJ6KGGwZ3nv[4Vv\XOrczDhd5NigSxiSVO1NF0xNjF{IN88US=> NI[wboI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe0NVI1QSd-MkG3OFEzPDl:L3G+
HEK293 M2\iOGZ2dmO2aX;uJIF{e2G7 NF\hO5BDcW6maX7nJIFn\mmwaYT5JJRwKE[OVEOgZ4F1[Wy7dHnjJIRwdWGrbjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHL5JINwdXCndHn0bZZmKGKrbnTpcoch[XO|YYmsJGtlKD1iMD6wNFA1PyEQvF2u NGLFbJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe1OFE6QSd-MUm3OVQyQTl:L3G+
MV4-11 M2\KV2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MmHWO|IhcHK| M2jTcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSmxVOy2LVFSg[IVx\W6mZX70JIh2dWGwIF3WOE0yOSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KGOnbHz0bZRmei2pbH:vR2NMQCCjc4PhfUwhT0l3MDC9JFAvODBzIN88UU4> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
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ES3 NEfERmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGVUOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iM{euOVAxPCEQvF2u MlL4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVM2Nyd-U1HOS2VTRC:jPh?=
NCI-H2141 NVO0PI44T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkG0NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOzhwMEi0N{DPxE1w NXLsUHdCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
MPP-89 M323eWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHPTY5pcWKrdHnvckBw\iCqdX3hckBOWFBvOEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQzNjB3OE[g{txONg>? NWXVVYtJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
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LC-1F M33jdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4\hPWlvcGmkaYTpc44hd2ZiaIXtZY4hVENvMV[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ{NjN4OEKg{txONg>? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-
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RKO MlqxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3m0fWlvcGmkaYTpc44hd2ZiaIXtZY4hWkuRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0OE4yOjV{IN88UU4> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
p-AKT / AKT / p-ERK / ERK ; 

PubMed: 24759734     


Effect of 72 h treatment with sunitinib on SH-SY5Y, SK N BE(2), SK-N-AS and IMR-32 NB cell lines analyzed by Western blot with pSer(473)Akt, Akt, pThr202/Thr204 Erk1/2 and Erk1/2 antibodies. β-actin was used as a loading control.

p-GSK3β / GSK3β / MYCN ; 

PubMed: 24759734     


Effect of sunitinib on GSK3β phosphorylation and on MYCN total protein in MYCN amplified NB cell lines.

p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 19244102     


Sunitinib reduced Stat3 and Src activity, with no dramatic reduction of AKT, MAPK and JAK signaling in 786-O cells. Tumor cells were treated with sunitinib at indicated concentrations for 2 h (left panels) or 24 h (right panels). Total cell lysates were prepared and western blots were performed using relevant antibodies to detect total protein levels, with β-actin used as the loading control.

24759734 19244102
Growth inhibition assay
Cell viability; 

PubMed: 24369536     


Isolated effects of sunitinib malate on urinary bladder-cancer cell lines viability, assessed by using the MTT assay. The data shown and bars represent the mean values ± SD (SD: standard deviation). *P < 0.05 versus untreated cells.

24369536
体内試験 Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferase fusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
細胞試験:

[3]

- 合併
  • 細胞株: RS4;11, MV4;11, and OC1-AML5
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間: 24 and 48 hours
  • 実験の流れ:

    Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.


    (参考用のみ)
動物試験:

[2]

- 合併
  • 動物モデル: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • 投薬量: ~80 mg/kg
  • 投与方法: Orally once daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 25 mg/mL (62.73 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+corn oil
混合させたのち直ちに使用することを推奨します。
0.875mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 398.47
化学式

C22H27FN4O2

CAS No. 557795-19-4
Storage powder
in solvent
別名 SU11248
Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04669366 Not yet recruiting Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer December 15 2020 --
NCT04633122 Recruiting Drug: Ripretinib|Drug: Sunitinib Gastrointestinal Stromal Tumor(GIST) Zai Lab (Shanghai) Co. Ltd. November 25 2020 Phase 2
NCT04115189 Active not recruiting Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT03916458 Completed -- Carcinoma Renal Cell Pfizer December 17 2019 --
NCT04033991 Active not recruiting Drug: Sunitinib|Drug: Axitinib Carcinoma|Renal Cell Pfizer September 27 2019 --
NCT03900793 Recruiting Drug: Losartan|Drug: Sunitinib Osteosarcoma University of Colorado Denver|National Cancer Institute (NCI) August 22 2019 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

PDGFRシグナル伝達経路

相関PDGFR製品

Tags: Sunitinibを買う | Sunitinib ic50 | Sunitinib供給者 | Sunitinibを購入する | Sunitinib費用 | Sunitinib生産者 | オーダーSunitinib | Sunitinib化学構造 | Sunitinib分子量 | Sunitinib代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID